KR101456994B1 - 안드로겐 수용체 길항제 및 그의 용도 - Google Patents

안드로겐 수용체 길항제 및 그의 용도 Download PDF

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KR101456994B1
KR101456994B1 KR1020127007933A KR20127007933A KR101456994B1 KR 101456994 B1 KR101456994 B1 KR 101456994B1 KR 1020127007933 A KR1020127007933 A KR 1020127007933A KR 20127007933 A KR20127007933 A KR 20127007933A KR 101456994 B1 KR101456994 B1 KR 101456994B1
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통유지
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/72Two oxygen atoms, e.g. hydantoin
    • C07D233/76Two oxygen atoms, e.g. hydantoin with substituted hydrocarbon radicals attached to the third ring carbon atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41661,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41781,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28Antiandrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/86Oxygen and sulfur atoms, e.g. thiohydantoin
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • General Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Engineering & Computer Science (AREA)
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  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020127007933A 2009-09-10 2010-09-08 안드로겐 수용체 길항제 및 그의 용도 KR101456994B1 (ko)

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Application Number Priority Date Filing Date Title
US24105109P 2009-09-10 2009-09-10
US61/241,051 2009-09-10
PCT/CN2010/076726 WO2011029392A1 (en) 2009-09-10 2010-09-08 Androgen receptor antagonists and uses thereof

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KR20120048705A KR20120048705A (ko) 2012-05-15
KR101456994B1 true KR101456994B1 (ko) 2014-11-04

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US (2) US8809550B2 (ja)
EP (1) EP2475647B1 (ja)
JP (1) JP5659232B2 (ja)
KR (1) KR101456994B1 (ja)
CN (2) CN102757389B (ja)
CA (1) CA2772579C (ja)
IN (1) IN2012DN02057A (ja)
WO (1) WO2011029392A1 (ja)
ZA (1) ZA201202029B (ja)

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UY34646A (es) 2012-03-02 2013-10-31 Novartis Ag Compuestos de espirohidantoína y su uso como moduladores selectivos del receptor de andrógenos
US9944607B2 (en) 2012-10-16 2018-04-17 Whitehead Institute For Biomedical Research Thiohydantoin derivatives and uses thereof
WO2014078929A1 (pt) * 2012-11-26 2014-05-30 Universidade Federal De Minas Gerais - Ufmg Formulações tópicas para a prevenção e tratamento da alopecia e para inibição do crescimento de pêlos
CN103304439B (zh) * 2013-06-04 2015-08-12 常州大学 一种4-氨基-2-氟-n-甲基苯甲酰胺的制备方法
CN104803919A (zh) * 2014-01-26 2015-07-29 上海医药工业研究院 用于制备恩杂鲁胺中间体的方法
CN103896847B (zh) * 2014-04-09 2016-01-20 沈江 一种非甾体类抗雄激素化合物及其制备方法和应用
CN103910679B (zh) * 2014-04-23 2016-05-25 杭州新博思生物医药有限公司 一种恩杂鲁胺的制备方法
CN104003939B (zh) * 2014-06-06 2017-07-07 山东大学 二芳基取代乙内酰硫脲类化合物及其制备方法与应用
CA2967195A1 (en) * 2014-11-10 2016-05-19 Glaxosmithkline Intellectual Property (No.2) Limited Long acting pharmaceutical compositions for hepatitis c
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US20190209469A1 (en) * 2016-08-20 2019-07-11 Ftf Pharma Private Limited Pharmaceutical composition comprising an androgen receptor inhibitor
RU2733950C1 (ru) * 2017-02-13 2020-10-08 Канпу Биофармасьютикалс, Лтд. Комбинация для лечения рака предстательной железы, фармацевтическая композиция и способ лечения
CN109700794B (zh) * 2017-03-01 2021-01-08 浙江大学 腙结构类型雄激素受体拮抗剂及其应用
US11292782B2 (en) 2018-11-30 2022-04-05 Nuvation Bio Inc. Diarylhydantoin compounds and methods of use thereof
US20210323931A1 (en) * 2020-04-17 2021-10-21 Essa Pharma, Inc. Solid forms of an n-terminal domain androgen receptor inhibitor and uses thereof
US20230233690A1 (en) * 2020-07-10 2023-07-27 The Regents Of The University Of Michigan Androgen receptor protein degraders
CN112876391A (zh) * 2021-01-15 2021-06-01 山东铂源药业有限公司 一种4-异硫氰基-2-(三氟甲基)苯甲腈的合成方法
CN113024513A (zh) * 2021-03-22 2021-06-25 中国药科大学 新型雄激素受体降解剂、制备方法和医药用途
CN115109031A (zh) * 2021-03-23 2022-09-27 苏州开拓药业股份有限公司 雄激素受体拮抗剂的无水多晶型物及其制备方法和用途
CN115583898A (zh) * 2021-07-06 2023-01-10 苏州开拓药业股份有限公司 一种异硫氰酸芳基酯的制备方法
CN114014850A (zh) * 2021-12-17 2022-02-08 山东汇海医药化工有限公司 一种普克鲁胺中间体及其合成方法及由该中间体合成普克鲁胺的方法
CN114181155A (zh) * 2021-12-21 2022-03-15 上海朝晖药业有限公司 碘-恩杂鲁胺及其制备方法及其应用
CN115181043B (zh) * 2022-07-27 2024-05-07 爱斯特(成都)生物制药股份有限公司 一种连续流制备4-异硫氰基-2-(三氟甲基)苯甲腈的方法
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EP2475647A1 (en) 2012-07-18
CN102482230B (zh) 2016-01-06
WO2011029392A1 (en) 2011-03-17
JP5659232B2 (ja) 2015-01-28
JP2013504522A (ja) 2013-02-07
EP2475647A4 (en) 2013-03-27
EP2475647B1 (en) 2015-11-04
CN102757389A (zh) 2012-10-31
CA2772579C (en) 2015-12-08
US20140315957A1 (en) 2014-10-23
CN102482230A (zh) 2012-05-30
ZA201202029B (en) 2012-11-28
KR20120048705A (ko) 2012-05-15
US20120172406A1 (en) 2012-07-05
US8809550B2 (en) 2014-08-19
CN102757389B (zh) 2015-07-08
CA2772579A1 (en) 2011-03-17
IN2012DN02057A (ja) 2015-08-21

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